ArticlePharmaceutical research1998
Correlation between oral drug absorption in humans, and apparent drug permeability in TC-7 cells, a human epithelial intestinal cell line: comparison with the parental Caco-2 cell line.
Article in Pharmaceutical research, 1998. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 38 papers.
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Who cites it
38 citing papers in PubMed, 238 citations in OpenAlex.
- Effect of the main dietary antioxidants (carotenoids, gamma-tocopherol, polyphenols, and vitamin C) on alpha-tocopherol absorption.European journal of clinical nutrition · 2007Trial
- Improving the Accuracy of Permeability Data to Gain Predictive Power: Assessing Sources of Variability in Assays Using Cell Monolayers.Membranes · 2024Review
- Flavonoids in the Spotlight: Bridging the Gap between Physicochemical Properties and Formulation Strategies.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Analyzing the metabolic fate of oral administration drugs: A review and state-of-the-art roadmap.Frontiers in pharmacology · 2022Review
- Characterization of three naturally occurring lignans, sesamol, sesamolin, and sesamin, as potent inhibitors of human cytochrome P450 46A1: Implications for treating excitatory neurotoxicity.Frontiers in pharmacology · 2022Article
- Drug Penetration into the Central Nervous System: Pharmacokinetic Concepts and In Vitro Model Systems.Pharmaceutics · 2021Review
- Article
- Rifabutin-Loaded Nanostructured Lipid Carriers as a Tool in Oral Anti-Mycobacterial Treatment of Crohn's Disease.Nanomaterials (Basel, Switzerland) · 2020Article
- Development of an Improved 3DFrontiers in bioengineering and biotechnology · 2020Article
- Soy-derived phytoalexins: mechanism of in vivo biological effectiveness in spite of their low bioavailability.Food science and biotechnology · 2019Review
- Incorporating physiologically relevant mobile phases in micellar liquid chromatography for the prediction of human intestinal absorption.Biomedical chromatography : BMC · 2018Article
- Influence of PEGylation of Vitamin-K-Loaded Mixed Micelles on the Uptake by and Transport through Caco-2 Cells.Molecular pharmaceutics · 2018Article
- Development of a Dynamic Physiologically Based Mechanistic Kidney Model to Predict Renal Clearance.CPT: pharmacometrics & systems pharmacology · 2018Article
- Synthesis and characterization of chitosan-grafted-polycaprolactone micelles for modulate intestinal paclitaxel delivery.Drug delivery and translational research · 2018Article
- Self-assembled α-Tocopherol Transfer Protein Nanoparticles Promote Vitamin E Delivery Across an Endothelial Barrier.Scientific reports · 2017Article
- Drug-transporter mediated interactions between anthelminthic and antiretroviral drugs across the Caco-2 cell monolayers.BMC pharmacology & toxicology · 2017Article
- Prediction of the permeability of neutral drugs inferred from their solvation properties.Bioinformatics (Oxford, England) · 2016Article
- Effects of silver nanoparticles and ions on a co-culture model for the gastrointestinal epithelium.Particle and fibre toxicology · 2016Article
- Development and validation of an UPLC-MS/MS method for the quantification of columbin in biological matrices: Applications to absorption, metabolism, and pharmacokinetic studies.Journal of chromatography. B, Analytical technologies in the biomedical and life sciences · 2015Article
- TEER measurement techniques for in vitro barrier model systems.Journal of laboratory automation · 2015Review
Corrections and comments
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo determine and compare the relationship between in vivo oral absorption in humans and the apparent permeability coefficients (Papp) obtained in vitro on two human intestinal epithelial cell lines, the parental Caco-2 and the TC-7 clone.
methodsBoth cell lines were grown for 5-35 days on tissue culture-treated inserts. Cell monolayers were analysed for their morphology by transmission electron micrography, and for their integrity with respect to transepithelial electrical resistance, mannitol and PEG-4000 transport, and cyclosporin efflux. Papp were determined for 20 compounds exhibiting large differences in chemical structure, molecular weight, transport mechanisms, and percentage of absorption in humans.
resultsThe TC-7 clone exhibits morphological characteristics similar to those of the parental Caco-2 cell line, concerning apical brush border, microvilli, tight junctions and polarisation of the cell line. The TC-7 clone however appeared more homogenous in terms of cell size. Both cell lines achieved a similar monolayer integrity towards mannitol and PEG-4000. Monolayer integrity was achieved earlier for the TC-7 clone, mainly due to its shorter doubling time, i.e. 26 versus 30 hours for parental Caco-2 cells. When using cyclosporin A as a P-glycoprotein substrate, active efflux was lower in the TC-7 clone than in the parental Caco-2 cells. The Papp and mechanisms of transport (paracellular or transcellular routes, passive diffusion and active transport) were determined for 20 drugs. A relationship was established between the in vivo oral absorption in humans and Papp values, allowing to determine a threshold value for Papp of 2 10(-6) cm/sec, above for which a 100% oral absorption could be expected in humans. Both correlation curves obtained with the two cell types, were almost completely superimposable. These studies also confirmed that the dipeptide transporter is underexpressed in both cell lines.
conclusionsOn the basis of morphological parameters, biochemical activity and drug transport characteristics, the TC-7 clone appeared to be a valuable alternative to the use of parental Caco-2 cells for drug absorption studies.
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